Synthesis of 3,5-Bis(trifluoromethyl)phenyl-Substituted Pyrazole Derivatives as Potent Growth Inhibitors of Drug-Resistant Bacteria
Enterococci and methicillin-resistant <i>S. aureus</i> (MRSA) are among the menacing bacterial pathogens. Novel antibiotics are urgently needed to tackle these antibiotic-resistant bacterial infections. This article reports the design, synthesis, and antimicrobial studies of 30 novel pyr...
| Main Authors: | , , , , , |
|---|---|
| Format: | Article |
| Language: | English |
| Published: |
MDPI AG
2021-08-01
|
| Series: | Molecules |
| Subjects: | |
| Online Access: | https://www.mdpi.com/1420-3049/26/16/5083 |
| _version_ | 1827684536747556864 |
|---|---|
| author | Ibrahim S. Alkhaibari Hansa Raj KC Subrata Roy Mohd. K. Abu-gazleh David F. Gilmore Mohammad A. Alam |
| author_facet | Ibrahim S. Alkhaibari Hansa Raj KC Subrata Roy Mohd. K. Abu-gazleh David F. Gilmore Mohammad A. Alam |
| author_sort | Ibrahim S. Alkhaibari |
| collection | DOAJ |
| description | Enterococci and methicillin-resistant <i>S. aureus</i> (MRSA) are among the menacing bacterial pathogens. Novel antibiotics are urgently needed to tackle these antibiotic-resistant bacterial infections. This article reports the design, synthesis, and antimicrobial studies of 30 novel pyrazole derivatives. Most of the synthesized compounds are potent growth inhibitors of planktonic Gram-positive bacteria with minimum inhibitory concertation (MIC) values as low as 0.25 µg/mL. Further studies led to the discovery of several lead compounds, which are bactericidal and potent against MRSA persisters. Compounds <b>11</b>, <b>28</b>, and <b>29</b> are potent against <i>S. aureus</i> biofilms with minimum biofilm eradication concentration (MBEC) values as low as 1 µg/mL. |
| first_indexed | 2024-03-10T08:32:36Z |
| format | Article |
| id | doaj.art-c599fde3f11d4154ba971c52639a4c24 |
| institution | Directory Open Access Journal |
| issn | 1420-3049 |
| language | English |
| last_indexed | 2024-03-10T08:32:36Z |
| publishDate | 2021-08-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj.art-c599fde3f11d4154ba971c52639a4c242023-11-22T08:56:24ZengMDPI AGMolecules1420-30492021-08-012616508310.3390/molecules26165083Synthesis of 3,5-Bis(trifluoromethyl)phenyl-Substituted Pyrazole Derivatives as Potent Growth Inhibitors of Drug-Resistant BacteriaIbrahim S. Alkhaibari0Hansa Raj KC1Subrata Roy2Mohd. K. Abu-gazleh3David F. Gilmore4Mohammad A. Alam5Department of Chemistry and Physics, The College of Sciences and Mathematics, Arkansas State University, Jonesboro, AR 72401, USADepartment of Chemistry and Physics, The College of Sciences and Mathematics, Arkansas State University, Jonesboro, AR 72401, USADepartment of Chemistry and Physics, The College of Sciences and Mathematics, Arkansas State University, Jonesboro, AR 72401, USADepartment of Chemistry and Physics, The College of Sciences and Mathematics, Arkansas State University, Jonesboro, AR 72401, USADepartment of Biological Sciences, The College of Sciences and Mathematics, Arkansas State University, Jonesboro, AR 72401, USADepartment of Chemistry and Physics, The College of Sciences and Mathematics, Arkansas State University, Jonesboro, AR 72401, USAEnterococci and methicillin-resistant <i>S. aureus</i> (MRSA) are among the menacing bacterial pathogens. Novel antibiotics are urgently needed to tackle these antibiotic-resistant bacterial infections. This article reports the design, synthesis, and antimicrobial studies of 30 novel pyrazole derivatives. Most of the synthesized compounds are potent growth inhibitors of planktonic Gram-positive bacteria with minimum inhibitory concertation (MIC) values as low as 0.25 µg/mL. Further studies led to the discovery of several lead compounds, which are bactericidal and potent against MRSA persisters. Compounds <b>11</b>, <b>28</b>, and <b>29</b> are potent against <i>S. aureus</i> biofilms with minimum biofilm eradication concentration (MBEC) values as low as 1 µg/mL.https://www.mdpi.com/1420-3049/26/16/5083pyrazoleaniline<i>Staphylococcus aureus</i><i>Enterococcus faecium</i>MRSA<i>Enterococcus faecalis</i> |
| spellingShingle | Ibrahim S. Alkhaibari Hansa Raj KC Subrata Roy Mohd. K. Abu-gazleh David F. Gilmore Mohammad A. Alam Synthesis of 3,5-Bis(trifluoromethyl)phenyl-Substituted Pyrazole Derivatives as Potent Growth Inhibitors of Drug-Resistant Bacteria Molecules pyrazole aniline <i>Staphylococcus aureus</i> <i>Enterococcus faecium</i> MRSA <i>Enterococcus faecalis</i> |
| title | Synthesis of 3,5-Bis(trifluoromethyl)phenyl-Substituted Pyrazole Derivatives as Potent Growth Inhibitors of Drug-Resistant Bacteria |
| title_full | Synthesis of 3,5-Bis(trifluoromethyl)phenyl-Substituted Pyrazole Derivatives as Potent Growth Inhibitors of Drug-Resistant Bacteria |
| title_fullStr | Synthesis of 3,5-Bis(trifluoromethyl)phenyl-Substituted Pyrazole Derivatives as Potent Growth Inhibitors of Drug-Resistant Bacteria |
| title_full_unstemmed | Synthesis of 3,5-Bis(trifluoromethyl)phenyl-Substituted Pyrazole Derivatives as Potent Growth Inhibitors of Drug-Resistant Bacteria |
| title_short | Synthesis of 3,5-Bis(trifluoromethyl)phenyl-Substituted Pyrazole Derivatives as Potent Growth Inhibitors of Drug-Resistant Bacteria |
| title_sort | synthesis of 3 5 bis trifluoromethyl phenyl substituted pyrazole derivatives as potent growth inhibitors of drug resistant bacteria |
| topic | pyrazole aniline <i>Staphylococcus aureus</i> <i>Enterococcus faecium</i> MRSA <i>Enterococcus faecalis</i> |
| url | https://www.mdpi.com/1420-3049/26/16/5083 |
| work_keys_str_mv | AT ibrahimsalkhaibari synthesisof35bistrifluoromethylphenylsubstitutedpyrazolederivativesaspotentgrowthinhibitorsofdrugresistantbacteria AT hansarajkc synthesisof35bistrifluoromethylphenylsubstitutedpyrazolederivativesaspotentgrowthinhibitorsofdrugresistantbacteria AT subrataroy synthesisof35bistrifluoromethylphenylsubstitutedpyrazolederivativesaspotentgrowthinhibitorsofdrugresistantbacteria AT mohdkabugazleh synthesisof35bistrifluoromethylphenylsubstitutedpyrazolederivativesaspotentgrowthinhibitorsofdrugresistantbacteria AT davidfgilmore synthesisof35bistrifluoromethylphenylsubstitutedpyrazolederivativesaspotentgrowthinhibitorsofdrugresistantbacteria AT mohammadaalam synthesisof35bistrifluoromethylphenylsubstitutedpyrazolederivativesaspotentgrowthinhibitorsofdrugresistantbacteria |